| Primary information |
|---|
| ID | 1846 |
| ThPP ID | Th1234 |
| Therapeutic Peptide/Protein Name | Protamine sulfate |
| Sequence | NA view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | NA |
| Chemical Formula | NA |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting Point (℃) | NA |
| Half Life | Without heparin in healthy individuals: Median 7.4 minutes. With heparin: Median 4.5 minutes. |
| Description | Protamine sulfate is a drug that reverses the anticoagulant effects of heparin by binding to it. It was originally isolated from the sperm of salmon and other species of fish but is now produced primarily through recombinant biotechnology. Protamine sulfate was approved for medical use in the United States in 1969. Protamine sulfate (protamine (protamines) s) occurs as fine white or off-white amorphous or crystalline powder. It is sparingly soluble in water. The pH is between 6 and 7. The cationic hydrogenated protamine at a pH of 6.8 to 7.1 reacts with anionic heparin at a pH of 5.0 to 7.5 to form an inactive complex. |
| Indication/Disease | Protamine sulfate is usually administered to reverse the large dose of heparin administered during certain surgeries, especially heart surgery. |
| Pharmacodynamics | Protamine sulphate 1% demonstrates activity neutralising anticoagulant properties of heparin, creating the complex heparin/protamine. Activity of protamine (towards heparin) takes place within five minutes after intravenous injection of the preparation. |
| Mechanism of Action | It is a highly cationic peptide that binds to either heparin or low molecular weight heparin (LMWH) to form a stable ion pair, which does not have anticoagulant activity. The ionic complex is then removed and broken down by the reticuloendothelial system. In large doses, protamine sulfate may also have an independent—however weak—anticoagulant effect. |
| Toxicity | Administration of protamine sulfate intravenously could result in severe drop in blood pressure, dyspnea, bradycardia, pulmonary hypertension and anaphylaxis. Systemic hypertension, nausea, vomiting and lassitude were also reported. Overdosage of this drug may theoretically result in hemorrhage. |
| Metabolism | Metabolic fate of the protamine-heparin complex has not been elucidated; however, protamine-heparin complex may be partially metabolized or attacked by fibrinolysin, freeing heparin. |
| Absorption | After IV adminsteration, protamine sulfate takes less than 5 min. to neutralize heparin. |
| Volume of Distribution | 12.3 L |
| Clearance | Clearance is: 2.2 L/min |
| Categories | Heparin Antagonists, Hematologic Agents |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | NA |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Protamine Sulfate Injection, USP |
| Company | Omega Laboratories Ltd |
| Brand Discription | Protamine Sulfate Injection, USP is a sterile, non-pyrogenic, isotonic solution of protamine sulfate in Water for Injection. It acts as a heparin antagonist. It is also a weak anticoagulant. Protamines are simple protein principles obtained from the sperm of salmon and certain other species of fish. Protamine (protamines) s have low molecular weight, are rich in arginine, and are strongly basic. |
| Prescribed for | Protamine Sulfate (protamine (protamines) s) Injection, USP is indicated in the treatment of heparin overdosage. |
| Chemical Name | NA |
| Formulation | Protamine sulfate 10 mg, sodium chloride 9 mg and Water for Injection q.s. Sulfuric acid and/or dibasic sodium phosphate (heptahydrate) may have been added for pH adjustment. |
| Physcial Appearance | off-white amorphous or crystalline powder |
| Route of Administration | Intravenous |
| Recommended Dosage | Protamine Sulfate (protamine (protamines) s) Injection,USP should be given by very slow intravenous injection in doses not to exceed 50 mg of protamine sulfate (protamine (protamines) s) in any 10-minute period |
| Contraindication | Protamine sulfate (protamine (protamines) s) is contraindicated in patients who have shown previous intolerance to the drug. |
| Side Effects | Intravenous injections of protamine (protamines) may cause a sudden fall in blood pressure, bradycardia, pulmonary hypertension, dyspnea, or transitory flushing and a feeling of warmth. There have been reports of anaphylaxis that resulted in respiratory embarrassment |
| Useful Link | http://www.rxlist.com/protamine-drug.htm |
| PubMed ID | 11867368, 11001169 |
| 3-D Structure | N.A. |